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首页-小分子抑制剂&激动剂-GPCR-mAChR-Deschloroclozapine
Deschloroclozapine

Chemical Structure : Deschloroclozapine

CAS No.: 1977-07-7

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Deschloroclozapine (DCZ)

货号: PC-20104Not For Human Use, Lab Use Only.

Deschloroclozapine (DCZ) is a high-affinity and selective agonist for muscarinic-based DREADDs, shows nanomolar affinity for [3H]QNB-labeled hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Deschloroclozapine (DCZ) is a high-affinity and selective agonist for muscarinic-based DREADDs, shows nanomolar affinity for [3H]QNB-labeled hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively.
DCZ shows negligible affinities for a large number of GPCRs, ion channels and transporters (Ki values of >100 nM) and relatively low affinities for a few endogenous receptors, including muscarinic acetylcholine (hM1Ki=83 nM, hM5Ki =55 nM) and serotonin receptors (5-HT2AKi = 87 nM).
DCZ selectively bound to and occupied DREADDs in both mice and monkeys.
Systemic delivery of low doses of DCZ (1 or 3 μg per kg) enhanced neuronal activity via hM3Dq within minutes in mice and monkeys.
Intramuscular injections of DCZ (100 μg per kg) reversibly induced spatial working memory deficits in monkeys expressing hM4Di in the prefrontal cortex.
DCZ represents a potent, selective, metabolically stable and fast-acting DREADD agonist with utility in both mice and nonhuman primates for a variety of applications.

物理化学性质&存储条件

分子量 292.39
分子式 C18H20N4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine

参考文献

1. Nagai Y, et al. Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys. Nat. Neurosci. 2020;23:1157–1167.

2. Miyakawa N, et al. Nat Commun. 2023 Feb 28;14(1):971.

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